Oxalyl chloride → HCID 71679715, compound

Participants

Reaction Steps

The title compound was prepared following the procedure described in Example-1 using 2-methyl-4-morpholinoquinazolin-8-amine (Intermediate-51, 100 mg, 0.41 mmol), 6-chloro-2-fluoro-3-(pivalamidomethyl)benzoic acid (Intermediate-2, 176 mg, 0.61 mmol), oxalyl chloride (115 mg, 0.92 mmol), DMF (1 drop) and DIPEA (159 mg, 1.23 mmol) in CH2Cl2 (5 mL) to afford 53 mg of the title product. 1H NMR (400 MHz, DMSO-d6): δ 10.36 (s, 1H), 8.69 (d, J=7.6 Hz, 1H), 8.14-8.11 (t, J=5.7 Hz, 1H), 7.76-7.74 (d, J=8.4 Hz, 1H), 7.50-7.46 (t, J=8.1 Hz, 1H), 7.42 (d, J=8.4 Hz, 1H), 7.37-7.33 (t, J=8.0 Hz, 1H), 4.30 (d, J=5.7 Hz, 2H), 3.77 (d, J=4.7 Hz, 2H), 3.73 (d, J=4.6 Hz, 2H), 3.30 (s, 3H), 1.13 (s, 9H); MS (m/z): 514.29 (M+H)+.

Provenance & Evidence